1. Technical Field of the Invention
The present invention relates to novel compounds that are useful industrial products, which compounds are ligands that are activators of the RAR receptors. This invention also relates to compositions containing said novel ligands and to their formulation into pharmaceutical compositions for administration in human or veterinary medicine, or, alternatively into cosmetic compositions and to the non-therapeutic use of these compositions.
2. Description of Background and/or Related and/or Prior Art
Compounds with activity of retinoid type (vitamin A and its derivatives) are widely described in the literature as having activity in cell proliferation and differentiation processes. These properties give this class of compounds high potential in the treatment or prevention of numerous pathologies, and more particularly in dermatology and cancer. Many biological effects of retinoids are mediated by modulating the nuclear retinoic acid receptors (RAR).
The RAR receptors activate transcription by binding to DNA sequence elements, known as RAR response elements (RARE), in the form of a heterodimer with the retinoid X receptors (known as RXRs).
Three subtypes of human RARs have been identified and described: RARα, RARβ and RARγ.
Chemical compounds with activating activity on receptors of RAR type are known from the prior art. Especially representative are the aromatic heterocyclic biaryl compounds described in EP-0-816,352 B1, which find applications in the treatment of dermatological, rheumatic, respiratory and ophthalmological complaints, conditions or afflictions and also in the cosmetics field.
EP-0-661,258 describes biaromatic propynyl compounds more particularly containing an alkoxy substituent on the aromatic ring. This alkyl chain limits the solubility of the compounds.
Thus, need continues to exist for compounds with better solubility in water, with physicochemical and pharmacokinetic properties that are more suitable for application as medicinal products or cosmetics for man; this better solubility would also allow greater ease of formulation of the active principle in a composition.